Departments of Chemistry, McGill University, Montreal, Quebec, H3A 2K6, Canada.
J Med Chem. 2010 Oct 28;53(20):7461-5. doi: 10.1021/jm1007159.
Vitamin D receptor (VDR) antagonists have therapeutic potential in treatment of allergic conditions and hypercalcemia driven by granulomatous diseases. We have identified an o-aminoanilide analogue of the hormonal form of vitamin D with a dienyl side chain that functions as a strong VDR antagonist. Modeling studies indicate that antagonism arises from side chain rigidity, when compared to a more flexible saturated analogue, which interferes with H12 folding/alignment.
维生素 D 受体 (VDR) 拮抗剂在治疗过敏疾病和由肉芽肿性疾病引起的高钙血症方面具有治疗潜力。我们已经鉴定出一种维生素 D 激素形式的邻氨基苯甲酰胺类似物，具有二烯侧链，可作为强 VDR 拮抗剂。建模研究表明，与更具弹性的饱和类似物相比，拮抗作用源于侧链的刚性，后者干扰 H12 的折叠/排列。
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